ACS Medicinal Chemistry Letters · 2012 · 25 citations · 30 references
MedicineMedicinal ChemistryPharmacologyDrug DiscoveryMolecular PharmacologyNeuropharmacologyFluorescence ImagingFluorescence MicroscopyLigand BindingMolecular Probe DevelopmentReceptor ImagingReceptor PharmacologyConfocal Fluorescence MicroscopyConfocal Laser Scanning MicroscopyDopamine Receptor SubtypesFluorescence ProbesFluorescent Chemical ProbesFluorescent LabelsFluorescent ProbesHistamine Receptors
A piperidine-based lead structure for the human histamine H3 receptor (hH3R) was coupled with the BODIPY fluorophore and resulted in a strong green fluorescent (quantum yield, 0.92) hH3R ligand with affinity in the nanomolar concentration range (K i hH3R = 6.51 ± 3.31 nM), named Bodilisant. Screening for affinities at histamine and dopamine receptor subtypes showed high hH3R preference. Bodilisant was used for visualization of hH3R in hH3R overexpressing HEK-293 cells with fluorescence confocal laser scanning microscopy. In addition, in native human brain tissues, Bodilisant showed clear and displaceable images of labeled hH3R.
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